Enisamium is a small molecule inhibitor of the influenza A virus and SARS-CoV-2 RNA polymerases.

BioRxiv : the Preprint Server for Biology
Alexander P WalkerAartjan J W Te Velthuis

Abstract

Influenza A virus and coronavirus strains cause a mild to severe respiratory disease that can result in death. Although vaccines exist against circulating influenza A viruses, such vaccines are ineffective against emerging pandemic influenza A viruses. Currently, no vaccine exists against coronavirus infections, including pandemic SARS-CoV-2, the causative agent of the Coronavirus Disease 2019 (COVID-19). To combat these RNA virus infections, alternative antiviral strategies are needed. A key drug target is the viral RNA polymerase, which is responsible for viral RNA synthesis. In January 2020, the World Health Organisation identified enisamium as a candidate therapeutic against SARS-CoV-2. Enisamium is an isonicotinic acid derivative that is an inhibitor of multiple influenza B and A virus strains in cell culture and clinically approved in 11 countries. Here we show using in vitro assays that enisamium and its putative metabolite, VR17-04, inhibit the activity of the influenza virus and the SARS-CoV-2 RNA polymerase. VR17-04 displays similar efficacy against the SARS-CoV-2 RNA polymerase as the nucleotide analogue remdesivir triphosphate. These results suggest that enisamium is a broad-spectrum small molecule inhibitor of RNA ...Continue Reading

Citations

Jan 14, 2021·The Biochemical Journal·George M Burslem
Feb 10, 2021·Antimicrobial Agents and Chemotherapy·Aartjan J W Te VelthuisV. Margitich
Apr 16, 2021·The Journal of General Virology·Thomas P PeacockWendy S Barclay

Methods Mentioned

BETA
FCS
transfection
Tandem Affinity Purification

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